# US 10,869,933 B2 · Oligomer-phenothiazine conjugates

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- Number: US 10,869,933 B2
- Document ID: US10869933B2
- Status: Granted
- Kind: B2
- Application number: 16/599,605
- Filed: 2019-10-11
- Published: 2020-02-06
- Granted: 2020-12-22
- Earliest claimed: 2009-01-28
- Assignees: Nektar Therapeutics
- Applicants: Nektar Therapeutics
- Inventors: Xuyuan Gu; Jennifer Riggs-Sauthier
- Web page: https://patentgrep.com/patent/US10869933B2

## CPC

- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- A61P 1/08: for nausea, cinetosis or vertigo; Antiemetics
- A61P 1/12: Antidiarrhoeals
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/20: Hypnotics; Sedatives
- A61P 25/22: Anxiolytics
- A61P 35/00: Antineoplastic agents
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention relates to (among other things) oligomer-phenothiazine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over un-conjugated phenothiazine compounds.

## Claims

### Claim 1

A method of treating allergic reactions, anaphylaxis, motion sickness, nausea, or visceral pain comprising administering to a subject in need thereof a therapeutically effective amount of a compound having the formula:
R1, R2, R3, and R4, each independently are selected from the group consisting of hydrogen, unsubstituted alkyl, and substituted alkyl; or R3 and R4 together with the nitrogen form a heterocycle;
n is an integer equal to or greater than one;
X is a spacer moiety; and
POLY is a poly(ethylene oxide) polymer.

### Claim 2 (depends on 1)

The method of claim 1, wherein said administering is selected from parenteral, oral, transdermal, and rectal.

### Claim 3 (depends on 2)

The method of claim 2, wherein said parenteral administering is selected from intravenous and intramuscular injection.

### Claim 4 (depends on 1)

The method of claim 1, wherein said administering is orally administering.

### Claim 5 (depends on 1)

The method of claim 1, wherein administering comprises administering about 0.001 mg/day to 1000 mg/day.

### Claim 6 (depends on 1)

The method of claim 1, wherein administering comprises administering about 0.10 mg/day to 500 mg/day.

### Claim 7 (depends on 1)

The method of claim 1, wherein administering comprises administering on a dosing schedule selected from five times a day, four times a day, three times a day, twice daily, once daily, three times weekly, and twice weekly.

### Claim 8 (depends on 1)

The method of claim 1, wherein the poly(ethylene oxide) is a poly(ethylene glycol) polymer.

### Claim 9 (depends on 1)

The method of claim 1, wherein the poly(ethylene oxide) is made of from about 1 to about 30 monomers.

### Claim 10 (depends on 9)

The method of claim 9, wherein the poly(ethylene oxide) is made of from about 1 to about 10 monomers.

### Claim 11 (depends on 1)

The method of claim 1, wherein an alkoxy or hydroxy end-capping moiety is attached to the poly(ethylene oxide) polymer.

### Claim 12 (depends on 1)

The method of claim 1, wherein a single poly(ethylene oxide) polymer is attached to the phenothiazine residue.

### Claim 13 (depends on 1)

The method of claim 1, wherein more than one poly(ethylene oxide) polymer is attached to the phenothiazine residue.

### Claim 14 (depends on 1)

The method of claim 1, wherein the linkage is selected from an ether linkage and an ester linkage.

### Claim 15 (depends on 1)

The method of claim 1, wherein POLY is —(CH2CH2O)nY, wherein Y is selected from H and —CH3; and
n is 1 to 30.

### Claim 16 (depends on 1)

The method of claim 1, wherein X is —O— or a bond.

### Claim 17 (depends on 1)

The method of claim 1, having the formula:

### Claim 18 (depends on 1)

The method of claim 1, having the formula: